Article
Single Peptide Backbone Surrogate Mutations to Regulate Angiotensin GPCR Subtype Selectivity.
Chemistry (Weinheim an der Bergstrasse, Germany) - 21 Aug 2020
Vrettos Eirinaios I, Valverde Ibai E, Mascarin Alba, Pallier Patrick N, Cerofolini Linda, Fragai Marco, Parigi Giacomo, Hirmiz Baydaa, Bekas Nick, Grob Nathalie M, Stylos Evgenios Κ, Shaye Hamidreza, Del Borgo Mark, Aguilar Marie-Isabel, Magnani Francesca, Syed Nelofer, Crook Timothy, Waqif Emal, Ghazaly Essam, Cherezov Vadim, Widdop Robert E, Luchinat Claudio, Michael-Titus Adina T, Mindt Thomas L, Tzakos Andreas G
Abstract excerpt
Mutating the side-chains of amino acids in a peptide ligand, with unnatural amino acids, aiming to mitigate its short half-life is an established approach. However, it is hypothesized that mutating specific backbone peptide bonds with bioisosters can be exploited not only to enhance the proteolytic stability of parent peptides, but also to tune its receptor subtype selectivity. Towards this end, four [Y]6...
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